ABSTRACT
OBJECTIVE To establish a method for the determination of plasma protein binding rate of imatinib and its metabolite（N-desmethyl imatinib ）and apply it to patients with gastrointestinal stromal tumor （GIST）.METHODS Using imatinib - d8 as the internal standard ，after being deproteinized methanol ，the sample was determined by equilibrium dialysis combined with liquid chromatography -tandem mass spectrometry . The free concentrations of imatinib and its metabolites in plasma of GIST patients were detected by the same method . RESULTS The protein binding rates of imatinib with albumin ，α1-acid glycoprotein and globulin at 120 ng/mL and 4 000 ng/mL were （92.5±1.0）% and（91.7±0.4）%，（56.6±2.0）% and（62.6±2.6）%，（56.3±3.1）% and （68.0±8.6）% ，respectively. The protein binding rates of N-desmethyl imatinib with albumin ，α1-acid glycoprotein and globulin at 60 ng/mL and 2 000 ng/mL were （90.6±3.5）% and（91.3±1.5）%，（54.1±5.1）% and（63.7±1.3）%，（56.2±7.6）% and（67.5±7.3）%，respectively. Compared with the low concentration group of imatinib （120 ng/mL）and its metabolite （60 ng/mL），the plasma protein binding rate of high concentration of imatinib （4 000 ng/mL）and its metabolite （2 000 ng/mL）with α1-acid glycoprotein and globulin was significantly increased （P＜ Δ基金项目 国家自然科学基金资助项目（No.81503160）；江苏省 0.05），but there was no signifi -cant difference with albumin 卫生健康发展研究中心 2021年度开放课题（No.JSHD2021004）；江苏 （P＞0.05）. In blank plasma ，the protein binding rates of imatinib（4 000 ng/mL）at high concentration and its metabolites（2 000 ng/mL）were significantly lower than those of low （120， 60 ng/mL） and medium （750， 375 ng/mL）concentration （P＜0.01）. Average protein binding rates of imatinib and its metabolite in plasma of GIST patients were （99.0±0.3）% and（99.2±0.3）%，respectively；the correlation coefficients between the concentrations of imatinib and its metabolites and the protein binding rates were －0.298 5 and －3.332 3，respectively（all P＜0.05）. CONCLUSIONS The method for determining the plasma protein binding rates of imatinib and its metabolites is successfully established . The plasma protein binding rates of imatinib and its metabolites in patients with GIST are negatively correlated with drug concentration .
ABSTRACT
Objective To observe the clinical efficacy of acupuncture at Jiaji (EX-B 2) points plus pelvic floor muscle exercises in treating postpartum stress urinary incontinence.Method A total of 216 patients with stress urinary incontinence were randomly divided into a treatment group and a control group, 108 cases each. The treatment group was intervened by acupuncture at Jiaji (EX-B 2) points plus pelvic floor muscle exercises, while the control group was intervened by pelvic flor muscle exercises alone. For the two groups, the treatment was given once a day, 12 sessions as a course. The total effective rates were compared after 2 treatment courses.Result The total effective rate was 90.7% in the treatment group versus 83.3% in the control group, and the difference was statistically significant (P<0.05).Conclusion Acupuncture at Jiaji (EX-B 2) points plus pelvic floor muscle exercises is an effective method in treating postpartum stress urinary incontinence, and can promote the postpartum recovery of the pelvic floor.
ABSTRACT
【Objective】To observe the effect of acupuncture mainly on cleft points on chemical radiculitis rats and to explore the therapeutic mechanism of acupuncture on lumbar disc prolapse.【Methods】Twenty-four rats with chemical radiculitis were equally randomized into acupuncture group and model group,and another 12 normal rats were in the blank control group.Acupuncture group received acupuncture on acupoints of Jiaji(EX-B2)and Weizhong(BL40)and cleft points of Foot-Shaoyang Meridian and Foot-Taiyang Meridian for 28 days.After treatment,rat behavioral changes and morphological features of nerve cells were observed,the weight of inflammation filter paper was detected,and hemorheologic parameters,nitric oxide (NO) and interleukin 6(IL-6) were assayed.【Results】Acupuncture improved the motor function of affected limb,recovered the senses of pain and tough,improved hemorheologic parameters,reduced the inflammatory reaction,relieved degeneration of nerve root,and decreased the contents of inflammatory factors(P